| 货号 | 16297-100mg |
| 描述 | The recurrent missense mutation T790M in the kinase domain of epidermal growth factor receptor (EGFR) is a gatekeeper mutation, as it sterically hinders binding of inhibitors while preserving catalytic activity.1,2 WZ4002 is an irreversible EGFR tyrosine kinase inhibitor that blocks ATP-dependent autophosphorylation of EGFR carrying the T790M mutation as well as an L858R mutation (IC50 = 8 nM).2,3 It preferentially targets cells expressing EGFRT790M over those expressing EGFR without the T790M mutation.2 WZ4002 is also bioavailable in vivo when given intravenously and is effective in mouse models of lung cancer driven by EGFRT790M.2 Efficacy may be enhanced when used in combination therapy with inhibitors of Met kinase activity, Bcl-2, or histone deacetylases.4,5,6,7 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Godin-Heymann, N.,Ulkus, L.,Brannigan, B.W., et al. The T790M "gatekeeper" mutation in EGFR mediates resistance to low concentrations of an irreversible EGFR inhibitor. Molecular Cancer Therapeutics 7(4), 874-879 (2008). 2.Zhou, W.,Ercan, D.,Chen, L., et al. Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. Nature 462(7276), 1070-1074 (2009). 3.Lee, H.J.,Schaefer, G.,Heffron, T.P., et al. Noncovalent wild-type-sparing inhibitors of EGFR T790M. Cancer Discov. 3(2), 168-181 (2013). 4.Wang, W.,Li, Q.,Takeuchi, S., et al. Met kinase inhibitor E7050 reverses three different mechanisms of hepatocyte growth factor-induced tyrosine kinase inhibitor resistance in EGFR mutant lung cancer. Clinical Cancer Research 18(6), 1663-1671 (2012). 5.Nakagawa, T.,Takeuchi, S.,Yamada, T., et al. Combined therapy with mutant-selective EGFR inhibitor and Met kinase inhibitor for overcoming erlotinib resistance in EGFR-mutant lung cancer. Molecular Cancer Therapeutics 11(10), 2149-2157 (2012). 6.Sakuma, Y.,Yamazaki, Y.,Nakamura, Y., et al. WZ4002, a third-generation EGFR inhibitor, can overcome anoikis resistance in EGFR-mutant lung adenocarcinomas more efficiently than Src inhibitors. Laboratory Investigation 92(3), 371-383 (2012). 7.Nanjo, S.,Yamada, T.,Nishihara, H., et al. Ability of the Met kinase inhibitor crizotinib and new generation EGFR inhibitors to overcome resistance to EGFR inhibitors. PLoS One 8(12), 1-13 (2013). | |
| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 495 |
| 分子式 | C25H27ClN6O3 |
| CAS号 | 1213269-23-8 |
| 稳定性 | ≥ 2 years |
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